Al technical title is built by PatSnap Al team. It summarizes the technical point description of the patent document.
a technology of pyridoxine and compound, which is applied in the field of new compounds having corticotropinreleasingfactor receptor antagonistic activity, can solve the problems of low utility value of medicaments, achieve excellent crf receptor antagonistic activity, satisfy pharmacological activity, and safety
Inactive Publication Date: 2006-07-18
EISIA R&D MANAGEMENT CO LTD
View PDF23 Cites 19 Cited by
Summary
Abstract
Description
Claims
Application Information
AI Technical Summary
This helps you quickly interpret patents by identifying the three key elements:
Problems solved by technology
Method used
Benefits of technology
Problems solved by technology
However, it must be said that, from a viewpoint of pharmacokinetics such as the chemical stability in vivo, the bioavailability and the transferability to brain, the utility value thereof as a medicament is low.
However, a medicament which shows the excellent CRF receptor antagonism, and satisfies the pharmacological activity, the dose, the safety etc. as a medicament and effectively acts clinically has not been found.
Method used
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more
Image
Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
Click on the blue label to locate the original text in one second.
Reading with bidirectional positioning of images and text.
[0188]3-Chloro-2-aminopyrazine (2.1 g, 16.2 mmol) and methyl 2-chloro-3-oxopentanoate (6.7 mL, 48.6 mmol) were mixed, and heated under stirring at 170° C. for 2 hours. After being allowed to cool, the unnecessary materials were filtered off and washed with ethyl acetate, and then filtrates were combined and evaporated. The resulting residue was purified by silica gel column chromatography (n-hexane:ethyl acetate=4:1) to give the title compound (0.99 g) as white crystals.
[0190]3-(2,4-Dichlorophenyl)-2-pyrazinamine (1.43 g, 6.0 mmol) was dissolved in chloroform (9 mL), N-chlorosuccinimide (0.96 g, 7.2 mmol) was added thereto, and the mixture was stirred by heating under reflux for 4 hours. After being allowed to cool, water was added to the reaction mixture, which was extracted with ethyl acetate. The organic layer was dried over anhydrous magnesium sulfate and evaporated. The resulting residue was purified by silica gel column chromatography (ethyl acetate:n-hexane=1:2) to give the title compound (1.54 g) as yellow crystals.
[0192]3-Bromo-5-methyl-2-pyrazineamine (3.5 g, 18.6 mmol) and methyl 2-chloro-3-oxopentanoate (6.7 mL, 48.6 mmol) were mixed, and the mixture was heated under stirring at 130° C. for 1 hour. After being allowed to cool, the unnecessary materials were filtered off and washed with ethyl acetate, and then the filtrates were combined and evaporated. The resulting residue was purified by silica gel column chromatography (n-hexane:ethyl acetate=3:1) to give the title compound (0.32 g) as pale yellow crystals.
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more
PUM
Property
Measurement
Unit
carbon number
aaaaa
aaaaa
carbon number
aaaaa
aaaaa
temperature
aaaaa
aaaaa
Login to view more
Abstract
The present invention provides a novel compound having an excellent corticotrophin-releasing-factor receptor antagonistic activity. That is, it provides a compound represented by the following formula or a salt thereof.Wherein R1 denotes a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group and the like; R2 denotes a halogen atom, a cyano group, a nitro group, a C1-10 alkyl group, a C2-10 alkenyl group, C2-10 alkynyl group and the like; R3 denotes a C6-14 aromatic hydrocarbon cyclic group or a 5- to 14-membered aromatic heterocyclic group, each of which may have a substituent; and X, Y and X are independent of each other and each denotes N or CR4 (wherein R4 denotes a hydrogen atom, a halogen atom, a cyano group, a nitro group, an optionally halogenated C1-6 alkyl group and the like) and, in this case, at least two of X, Y and Z denote CR4.
Description
[0001]This application is the national phase under 35 U.S.C. § 371 of PCT International Application No. PCT / JP02 / 01098 which has an International filing date of Feb. 8, 2002, which designated the United States of America.FIELD OF THE INVENTION[0002]The present invention relates to a novel compound having corticotropin-releasing-factor receptor antagonistic activity, a salt thereof and a hydrate of them, a process for preparing its and its medical use.PRIOR ART[0003]Corticotropin-releasing-factor (hereinafter, referred to as “CRF”) is a neuropeptide comprising 41 amino acids, and isolated from sheep hypothalamus (Science, 213, 1394 (1981)) and, then, its presence was confirmed in a rat (Proc. Natl. Acad. Sci. USA, 80, 4851 (1983)) and a human being (EMBO J. 5, 775 (1983)). CRF is the most abundant in pituitary gland and hypothalamus and is widely distributed in a brain such as cerebral cortex, cerebellum and the like. In addition, in a peripheral tissue, CRF is confirmed to be presen...
Claims
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more
Application Information
Patent Timeline
Application Date:The date an application was filed.
Publication Date:The date a patent or application was officially published.
First Publication Date:The earliest publication date of a patent with the same application number.
Issue Date:Publication date of the patent grant document.
PCT Entry Date:The Entry date of PCT National Phase.
Estimated Expiry Date:The statutory expiry date of a patent right according to the Patent Law, and it is the longest term of protection that the patent right can achieve without the termination of the patent right due to other reasons(Term extension factor has been taken into account ).
Invalid Date:Actual expiry date is based on effective date or publication date of legal transaction data of invalid patent.
![Imidazo[1,2-b]pyridazine compound](https://images-eureka.patsnap.com/patent_img/4b3d15b4-0b64-483b-bbe7-80e05715cba3/US07078405-20060718-C00001.png)
![Imidazo[1,2-b]pyridazine compound](https://images-eureka.patsnap.com/patent_img/4b3d15b4-0b64-483b-bbe7-80e05715cba3/US07078405-20060718-C00002.png)
![Imidazo[1,2-b]pyridazine compound](https://images-eureka.patsnap.com/patent_img/4b3d15b4-0b64-483b-bbe7-80e05715cba3/US07078405-20060718-C00003.png)
Login to view more